CUDC-101 [Ligand Id: 8894] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL598797 (Cudc 101, Cudc-101, CUDC-101)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 10/Histone deacetylase 10 in Human [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
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  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
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  • histone deacetylase 3/Histone deacetylase 3 in Human [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
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  • histone deacetylase 4/Histone deacetylase 4 in Human [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
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  • histone deacetylase 5/Histone deacetylase 5 in Human [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • histone deacetylase 7/Histone deacetylase 7 in Human [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
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  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
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  • histone deacetylase 9/Histone deacetylase 9 in Human [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
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  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR phosphorylation at Tyr1068 in human MDA-MB-468 cells B 7.75 pIC50 17.6 nM IC50 US-20080221132-A1. Multi-functional small molecules as anti-proliferative agents (2008)
ChEMBL Inhibition of EGFR B 8.62 pIC50 2.4 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
ChEMBL Inhibition of EGFR B 8.62 pIC50 2.4 nM IC50 J. Med. Chem. (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL Inhibition of recombinant human amino-terminal GST-His6-fused EGFR expressed in baculovirus expression system assessed as phosphorylation using Biotin-PTP1B as substrate by HTScan assay B 8.62 pIC50 2.4 nM IC50 Bioorg Med Chem (2017) 25: 27-37 [PMID:27769671]
ChEMBL Inhibition of N-terminal GST-fused human EGFR (His672 to Ala1210 residues) expressed in baculovirus expression system using biotinylated PTP1B at Tyr66 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by DELFIA B 8.62 pIC50 2.4 nM IC50 US-20080221132-A1. Multi-functional small molecules as anti-proliferative agents (2008)
ChEMBL Inhibition of EGFR (unknown origin) by HTscan assay B 8.62 pIC50 2.4 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
GtoPdb - - 8.62 pIC50 2.4 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of FGFR2 B 5.46 pIC50 3430 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of human HDAC1 expressed in Escherichia coli B 8.35 pIC50 4.5 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
GtoPdb - - 8.35 pIC50 4.5 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8]
ChEMBL Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay B 6.4 pIC50 398.11 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
ChEMBL Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay B 6.9 pIC50 125.89 nM IC50 J Med Chem (2019) 62: 4426-4443 [PMID:30964290]
GtoPdb - - 7.58 pIC50 26.1 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
ChEMBL Inhibition of human HDAC10 expressed in Escherichia coli B 7.58 pIC50 26.1 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of human HDAC2 expressed in Escherichia coli B 7.9 pIC50 12.6 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
GtoPdb - - 7.9 pIC50 12.6 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379]
GtoPdb - - 8.04 pIC50 9.1 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
ChEMBL Inhibition of human HDAC3 expressed in Escherichia coli B 8.04 pIC50 9.1 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524]
ChEMBL Inhibition of human HDAC4 expressed in Escherichia coli B 7.88 pIC50 13.2 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
GtoPdb - - 7.88 pIC50 13.2 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6]
GtoPdb - - 7.94 pIC50 11.4 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
ChEMBL Inhibition of human HDAC5 expressed in Escherichia coli B 7.94 pIC50 11.4 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
GtoPdb - - 8.29 pIC50 5.1 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
ChEMBL Inhibition of human HDAC6 expressed in Escherichia coli B 8.29 pIC50 5.1 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4]
ChEMBL Inhibition of human HDAC7 expressed in Escherichia coli B 6.43 pIC50 373 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
GtoPdb - - 6.43 pIC50 373 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Inhibition of human HDAC8 expressed in Escherichia coli B 7.1 pIC50 79.8 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
GtoPdb - - 7.1 pIC50 79.8 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0]
GtoPdb - - 7.17 pIC50 67.2 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
ChEMBL Inhibition of human HDAC9 expressed in Escherichia coli B 7.17 pIC50 67.2 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
ChEMBL Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 1817-1828 [PMID:28218840]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human HER2 (679 to 1255 residues) expressed in baculovirus infected insect Sf9 cells using poly (Glu:Tyr) 4:1 as substrate after 2 hrs B 6.73 pIC50 188 nM IC50 US-20080221132-A1. Multi-functional small molecules as anti-proliferative agents (2008)
ChEMBL Inhibition of N-terminal GST-tagged human HER2 (Lys676 to Val1255 residues) expressed in baculovirus expression system using biotinylated FLT3 at Tyr589 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by DELFIA method B 7 pIC50 100 nM IC50 US-20080221132-A1. Multi-functional small molecules as anti-proliferative agents (2008)
ChEMBL Inhibition of recombinant human amino-terminal GST-fused HER2 (Lys676-Val1255) expressed in baculovirus expression system using Biotin-FLT3 (Tyr589) peptide as substrate and ATP by HTScan assay B 7.79 pIC50 16.4 nM IC50 Bioorg Med Chem (2017) 25: 27-37 [PMID:27769671]
GtoPdb - - 7.8 pIC50 15.7 nM IC50 J Med Chem (2010) 53: 2000-9 [PMID:20143778]
ChEMBL Inhibition of HER2 B 7.8 pIC50 15.7 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
ChEMBL Inhibition of erbB2 B 7.8 pIC50 15.7 nM IC50 J. Med. Chem. (2010) 53: 1413-1437 [PMID:20166671]
ChEMBL Inhibition of HER2 (unknown origin) B 7.8 pIC50 15.7 nM IC50 J Med Chem (2019) 62: 3171-3183 [PMID:30418766]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of Abl1 B 5.54 pIC50 2890 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of Lck B 5.23 pIC50 5910 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of Lyn B 6.08 pIC50 840 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of Flt3 B 5.82 pIC50 1500 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of Ret B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of Src B 4.96 pIC50 11000 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of KDR B 6.07 pIC50 849 nM IC50 J. Med. Chem. (2010) 53: 2000-2009 [PMID:20143778]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]